Design and synthesis of oxytocin glycosides for the treatment of pain and substance use disorder

Hannah J. Goodman, Lajos Z. Szabò, Samuel M. Sugerman, Andriy Myloserdnyy, Robin Polt

Research output: Chapter in Book/Report/Conference proceedingChapter

Abstract

Peptide drugs are a promising alternative to classical small molecule therapeutics with diverse applications, ranging from antibiotic resistant infection to prostate cancer. Oxytocin (OT) is a highly evolutionarily conserved peptide neurohormone and has been of interest for pharmaceutical use since 1909. Despite their increased safety profile relative to most small molecule drugs, peptides are poor candidates based on the pharmacokinetic (PK) properties from their peptide nature. Broad application of OT as a drug has been limited by these same PK issues. Several strategies have been proposed to overcome these limitations, among them glycosylation, which was used in combination with other sequence modifications to produce robust antinociception in mouse models, increased selectivity and potency at the OT receptor, and improved stability in rats.

Original languageEnglish (US)
Title of host publicationPeptide and Peptide Mimicking Tools
Subtitle of host publicationMethods, Synthesis, Design
EditorsDavid Chenoweth
PublisherAcademic Press Inc.
Pages343-359
Number of pages17
ISBN (Print)9780443218149
DOIs
StatePublished - Jan 2024

Publication series

NameMethods in Enzymology
Volume698
ISSN (Print)0076-6879
ISSN (Electronic)1557-7988

Keywords

  • Antinociception
  • Glycopeptide
  • Glycosylation
  • Lactose
  • Neuropeptide
  • Oxytocin

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology

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